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Assay Detail

CHEMBL871108

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL ↗
46
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.
Imada T, Cho N, Imaeda T, Hayase Y, Sasaki S, Kasai S, Harada M, Matsumoto H, Endo S, Suzuki N, Furuya S.
J Med Chem (2006) 49 : 3809 -3825
PubMed 16789738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 7.94 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379629 — — 1 10.22
CHEMBL210294 — — 1 10.15
CHEMBL208812 — — 1 10.00
CHEMBL210709 — — 1 10.00
CHEMBL377396 — — 1 10.00
CHEMBL211485 — — 1 10.00
CHEMBL377015 — — 1 9.70
CHEMBL212121 — — 1 9.70
CHEMBL211503 — — 1 9.70
CHEMBL71917 — — 1 9.70
CHEMBL540109 — — 1 9.70
CHEMBL1201199 LEUPROLIDE 4.0 1 9.52
CHEMBL378979 — — 1 9.40
CHEMBL210321 — — 1 9.40
CHEMBL379198 — — 1 9.40
CHEMBL210888 — — 1 9.22
CHEMBL264121 — — 1 9.00
CHEMBL211098 — — 1 8.70
CHEMBL264574 — — 1 8.70
CHEMBL135103 — — 1 8.22
CHEMBL211731 — — 1 8.10
CHEMBL378481 — — 1 8.05
CHEMBL438652 — — 1 8.00
CHEMBL210277 — — 2 7.52
CHEMBL210295 — — 1 7.52
CHEMBL211808 — — 1 7.40
CHEMBL336319 — — 1 7.16
CHEMBL211588 — — 1 7.00
CHEMBL206964 — — 1 7.00
CHEMBL212207 — — 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379629 — IC50 = 0.06 nM 10.22
CHEMBL210294 — IC50 = 0.07 nM 10.15
CHEMBL210709 — IC50 = 0.1 nM 10.00
CHEMBL211485 — IC50 = 0.1 nM 10.00
CHEMBL377396 — IC50 = 0.1 nM 10.00
CHEMBL208812 — IC50 = 0.1 nM 10.00
CHEMBL212121 — IC50 = 0.2 nM 9.70
CHEMBL377015 — IC50 = 0.2 nM 9.70
CHEMBL540109 — IC50 = 0.2 nM 9.70
CHEMBL211503 — IC50 = 0.2 nM 9.70
CHEMBL71917 — IC50 = 0.2 nM 9.70
CHEMBL1201199 LEUPROLIDE IC50 = 0.3 nM 9.52
CHEMBL210321 — IC50 = 0.4 nM 9.40
CHEMBL379198 — IC50 = 0.4 nM 9.40
CHEMBL378979 — IC50 = 0.4 nM 9.40
CHEMBL210888 — IC50 = 0.6 nM 9.22
CHEMBL264121 — IC50 = 1.0 nM 9.00
CHEMBL264574 — IC50 = 2.0 nM 8.70
CHEMBL211098 — IC50 = 2.0 nM 8.70
CHEMBL135103 — IC50 = 6.0 nM 8.22
CHEMBL211731 — IC50 = 8.0 nM 8.10
CHEMBL378481 — IC50 = 9.0 nM 8.05
CHEMBL438652 — IC50 = 10.0 nM 8.00
CHEMBL210295 — IC50 = 30.0 nM 7.52
CHEMBL210277 — IC50 = 30.0 nM 7.52
CHEMBL210277 — IC50 = 30.0 nM 7.52
CHEMBL211808 — IC50 = 40.0 nM 7.40
CHEMBL336319 — IC50 = 70.0 nM 7.16
CHEMBL206964 — IC50 = 100.0 nM 7.00
CHEMBL211588 — IC50 = 100.0 nM 7.00
CHEMBL212051 — IC50 = 200.0 nM 6.70
CHEMBL212207 — IC50 = 200.0 nM 6.70
CHEMBL378845 — IC50 = 300.0 nM 6.52
CHEMBL378654 — IC50 = 300.0 nM 6.52
CHEMBL212472 — IC50 = 300.0 nM 6.52
CHEMBL208904 — IC50 = 400.0 nM 6.40
CHEMBL208714 — IC50 = 400.0 nM 6.40
CHEMBL211752 — IC50 = 500.0 nM 6.30
CHEMBL210845 — IC50 = 500.0 nM 6.30
CHEMBL209419 — IC50 = 700.0 nM 6.16
CHEMBL131751 — IC50 = 2000.0 nM 5.70
CHEMBL209880 — IC50 = 2000.0 nM 5.70
CHEMBL379274 — IC50 = 5000.0 nM 5.30
CHEMBL380200 — IC50 = 7000.0 nM 5.16
CHEMBL209836 — IC50 = 10000.0 nM 5.00
CHEMBL425051 — IC50 > 20000.0 nM -